US 7,514,451 B2
	7-(4-Substituted-3-cyclopropylaminomethyl-1 pyrrolidinyl) quinolonecarboxylic acid derivative
Yoshikazu Asahina, Tochigi (Japan); and Masaya Takei, Tochigi (Japan)
Assigned to Kyorin Pharmaceutical Co., Ltd., Tokyo (Japan)
Appl. No. 10/569,062 PCT Filed Sep. 08, 2004, PCT No. PCT/JP2004/013049 § 371(c)(1), (2), (4) Date Mar. 30, 2006, PCT Pub. No. WO2005/026147, PCT Pub. Date Mar. 24, 2005.
Claims priority of application No. 2003-318897 (JP), filed on Sep. 10, 2003.
Prior Publication US 2006/0281779 A1, Dec. 14, 2006
Int. Cl. C07D 471/02 (2006.01); C07D 215/38 (2006.01); A61K 31/44 (2006.01); A61K 31/47 (2006.01)

U.S. Cl. 514—312  [514/300; 546/123; 546/156]

20 Claims

1. A quinolonecarboxylic acid derivative represented by the following formula (I): wherein R1 is an alkyl group that has 1 to 6 carbon atoms and may or may not be substituted with 1 or 2 or more halogen atoms, a cycloalkyl group that has 3 to 6 carbon atoms and may or may not be substituted with 1 or 2 or more halogen atoms, or an aryl or heteroaryl group that may or may not be substituted with 1 or 2 or more substituents that are each independently a halogen atom or an amino group; R2 is a hydrogen atom, an alkyl group having 1 to 3 carbon atoms or pharmaceutically acceptable cation, R3 is a hydrogen atom, a halogen atom, a hydroxyl group, an amino group or an alkyl group having 1 to 3 carbon atoms; R4 is a hydrogen atom or a halogen atom; R5 is a fluorine atom; R6 is a hydrogen atom or a fluorine atom; and A is a nitrogen atom or =C-X, where X is a hydrogen atom, halogen atom, or alkyl or alkoxyl group that has 1 to 3 carbon atoms and may or may not be substituted with 1 or 2 or more amino groups, cyano groups or halogen atoms, or a salt thereof.